EA201170249A1 - 3,4-diarilpirazoly as protein kinase inhibitors - Google Patents

3,4-diarilpirazoly as protein kinase inhibitors

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Publication number
EA201170249A1
EA201170249A1 EA201170249A EA201170249A EA201170249A1 EA 201170249 A1 EA201170249 A1 EA 201170249A1 EA 201170249 A EA201170249 A EA 201170249A EA 201170249 A EA201170249 A EA 201170249A EA 201170249 A1 EA201170249 A1 EA 201170249A1
Authority
EA
Eurasian Patent Office
Prior art keywords
protein kinase
diarilpirazoly
kinase inhibitors
diarilpirazola
cancer
Prior art date
Application number
EA201170249A
Other languages
Russian (ru)
Unknown language (xx)
Other versions
EA019722B1 (en
Inventor
Маурицио Пуличи
Фабио Дзуккотто
Алессандра Бадари
Стефано Нуволони
Джованни Черви
Габриелла Тракванди
Соня Бьондаро
Паоло Трифиро'
Кьяра Маркионни
Микеле Модуньо
Original Assignee
НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP08161076 priority Critical
Application filed by НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. filed Critical НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л.
Priority to PCT/EP2009/059506 priority patent/WO2010010154A1/en
Publication of EA201170249A1 publication Critical patent/EA201170249A1/en
Publication of EA019722B1 publication Critical patent/EA019722B1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfasalazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems

Abstract

Раскрыты производные 3,4-диарилпиразола формулы (I), которые определены в описании, и их фармацевтически приемлемые соли, способ их получения и содержащие их фармацевтические композиции; Disclosed are derivatives of 3,4-diarilpirazola of formula (I), as defined herein, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions containing them; соединения согласно изобретению могут быть применимы в терапии, лечении заболеваний, ассоциированных с нарушенной регуляцией активности протеинкиназы, подобных злокачественной опухоли. compounds of the invention may be useful in therapy, the treatment of diseases associated with deregulated protein kinase activity, like cancer.
EA201170249A 2008-07-24 2009-07-23 3,4-diarylpyrazoles as protein kinase inhibitors EA019722B1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP08161076 2008-07-24
PCT/EP2009/059506 WO2010010154A1 (en) 2008-07-24 2009-07-23 3,4-diarylpyrazoles as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201170249A1 true EA201170249A1 (en) 2011-10-31
EA019722B1 EA019722B1 (en) 2014-05-30

Family

ID=41059486

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170249A EA019722B1 (en) 2008-07-24 2009-07-23 3,4-diarylpyrazoles as protein kinase inhibitors

Country Status (18)

Country Link
US (2) US8541575B2 (en)
EP (1) EP2324008B1 (en)
JP (1) JP5385382B2 (en)
CN (1) CN102105459B (en)
AT (1) AT557015T (en)
AU (1) AU2009273197B2 (en)
CA (1) CA2731146C (en)
CL (1) CL2011000124A1 (en)
CY (1) CY1117667T1 (en)
DK (1) DK2324008T3 (en)
EA (1) EA019722B1 (en)
ES (1) ES2386408T3 (en)
HK (1) HK1157337A1 (en)
HR (1) HRP20120577T1 (en)
MX (1) MX2011000738A (en)
PT (1) PT2324008E (en)
SI (1) SI2324008T1 (en)
WO (1) WO2010010154A1 (en)

Families Citing this family (30)

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Publication number Priority date Publication date Assignee Title
PE08372009A1 (en) 2007-07-02 2009-07-24 Boehringer Ingelheim Int New chemical compounds
ES2576684T3 (en) 2008-05-06 2016-07-08 Novartis Ag Oxazole and thiazole compounds benzenesulfonamide
AT557015T (en) * 2008-07-24 2012-05-15 Nerviano Medical Sciences Srl 3,4-diaryl pyrazoles as protein kinase inhibitors
CA2738448A1 (en) 2008-09-29 2010-04-01 Boehringer Ingelheim International Gmbh New chemical compounds
JP2011057661A (en) * 2009-08-14 2011-03-24 Bayer Cropscience Ag Pesticidal carboxamides
US8242260B2 (en) 2009-08-28 2012-08-14 Novartis Ag Compounds and compositions as protein kinase inhibitors
AR077975A1 (en) * 2009-08-28 2011-10-05 Irm Llc Pyrimidine and pyrazole derivatives compositions as protein kinase inhibitors
EP2528909B1 (en) 2010-01-27 2016-06-22 Nerviano Medical Sciences S.r.l. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
EP2552907B1 (en) 2010-03-26 2014-10-22 Boehringer Ingelheim International GmbH Pyridyltriazoles
WO2011117381A1 (en) 2010-03-26 2011-09-29 Boehringer Ingelheim International Gmbh B-raf kinase inhibitors
AR081810A1 (en) 2010-04-07 2012-10-24 Bayer Cropscience Ag bicyclic Piridinilpirazoles
CA2803055A1 (en) * 2010-06-25 2011-12-29 Novartis Ag Heteroaryl compounds and compositions as protein kinase inhibitors
EP2601185B1 (en) * 2010-08-03 2015-10-07 Nerviano Medical Sciences S.r.l. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents
TWI480276B (en) * 2010-08-27 2015-04-11 Irm Llc Compounds and compositions as protein kinase inhibitors
US8710055B2 (en) * 2010-12-21 2014-04-29 Boehringer Ingelheim International Gmbh Triazolylphenyl sulfonamides as serine/threonine kinase inhibitors
US8691184B2 (en) 2011-01-25 2014-04-08 The Regents Of The University Of Michigan Bcl-2/Bcl-xL inhibitors and therapeutic methods using the same
CN103403002B (en) 2011-02-24 2016-06-22 内尔维阿诺医学科学有限公司 As kinase inhibitors thiazolyl phenyl - phenyl sulfonylamino derivative
KR101298651B1 (en) * 2011-03-16 2013-08-21 연세대학교 산학협력단 Pharmaceutical Compositions for Enhanced Anti-angiogenic Activities
WO2013050437A1 (en) 2011-10-06 2013-04-11 Bayer Intellectual Property Gmbh Heterocyclylpyri (mi) dinylpyrazole as fungicidals
BR112014008222A2 (en) 2011-10-06 2017-04-25 Bayer Intelectual Property Gmbh heterociclilpiri (mi) dinilpirazol
HUE040370T2 (en) 2011-11-23 2019-03-28 Array Biopharma Inc Pharmaceutical formulations
CA2888960C (en) 2012-11-02 2017-08-15 Pfizer Inc. Bruton's tyrosine kinase inhibitors
SG11201505525UA (en) 2013-01-16 2015-08-28 Univ Michigan Bcl-2bcl-xl inhibitors and therapeutic methods using the same
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
UY36294A (en) 2014-09-12 2016-04-29 Novartis Ag Compounds and compositions as kinase inhibitors
EA201891268A1 (en) * 2015-12-16 2018-11-30 Локсо Онколоджи, Инк. Compounds which are useful as kinase inhibitors
CN106883266A (en) * 2017-01-23 2017-06-23 江苏七洲绿色化工股份有限公司 Preparation method of 1-(4-chlorphenyl)-2-cyclopropyl-1-cetone and intermediate thereof
WO2019081477A1 (en) 2017-10-26 2019-05-02 Bayer Cropscience Aktiengesellschaft Substituted pyrazoles, salts thereof and use thereof as herbicidal agents
WO2019081485A1 (en) 2017-10-26 2019-05-02 Bayer Cropscience Aktiengesellschaft Substituted pyrazoles, salts thereof and use thereof as herbicidal agents

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US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
EA003925B1 (en) 1997-05-22 2003-10-30 Дж.Д.Сирл Энд Ко SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
US7247734B2 (en) 2001-12-21 2007-07-24 Vernalis (Cambridge) Limited 3,4-diarylpyrazoles and their use in the therapy of cancer
BRPI0506760A (en) 2004-01-09 2007-05-22 Novartis Ag derivatives of phenyl- [4- (3-phenyl-1H-pyrazol-4-yl) -pyrimidin-2-yl] -amine as inhibitors of IGF-IR
JP2009506040A (en) 2005-08-26 2009-02-12 スミスクライン・ビーチャム・コーポレイションSmithkline Beecham Corporation Aurora kinases pyrimidinyl - pyrazole inhibitors
EP2024353A2 (en) * 2006-03-16 2009-02-18 Pfizer Products Inc. Pyrazole compounds
EP2057146A1 (en) * 2006-10-02 2009-05-13 Irm Llc Compounds and compositions as protein kinase inhibitors
AT557015T (en) * 2008-07-24 2012-05-15 Nerviano Medical Sciences Srl 3,4-diaryl pyrazoles as protein kinase inhibitors
EP2528909B1 (en) * 2010-01-27 2016-06-22 Nerviano Medical Sciences S.r.l. Sulfonamido derivatives of 3,4-diarylpyrazoles as protein kinase inhibitors
EP2601185B1 (en) 2010-08-03 2015-10-07 Nerviano Medical Sciences S.r.l. Derivatives of pyrazolophenyl-benzenesulfonamide compounds and use thereof as antitumor agents

Also Published As

Publication number Publication date
AU2009273197A1 (en) 2010-01-28
HRP20120577T1 (en) 2012-08-31
SI2324008T1 (en) 2012-08-31
EA019722B1 (en) 2014-05-30
PT2324008E (en) 2012-06-25
CL2011000124A1 (en) 2011-05-06
US8946250B2 (en) 2015-02-03
ES2386408T3 (en) 2012-08-20
AU2009273197B2 (en) 2014-01-16
CN102105459A (en) 2011-06-22
EP2324008B1 (en) 2012-05-09
CN102105459B (en) 2014-09-10
US20110144068A1 (en) 2011-06-16
JP5385382B2 (en) 2014-01-08
AU2009273197A2 (en) 2011-03-10
EP2324008A1 (en) 2011-05-25
WO2010010154A1 (en) 2010-01-28
CY1117667T1 (en) 2017-05-17
AT557015T (en) 2012-05-15
DK2324008T3 (en) 2012-07-23
CA2731146C (en) 2016-05-03
US8541575B2 (en) 2013-09-24
US20140005150A1 (en) 2014-01-02
MX2011000738A (en) 2011-02-23
CA2731146A1 (en) 2010-01-28
JP2011528698A (en) 2011-11-24
HK1157337A1 (en) 2013-02-15

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